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安定对兔心乳头肌动作电位和收缩的作用
EFFECTS OF DIAZEPAM ON THE ACTION POTENTIAL AND CONTRACTILITY OF RABBIT PAPILLARY MUSCLE
【摘要】 本文观察了安定、戊脉安和PK11195对兔心乳头肌动作电位和收缩的作用,并比较了安定对兔与豚鼠心肌收缩作用的差异。安定(0.7×10-6-22.4×10-6mol/L)使兔乙乳头肌动作电位时程(APD)及钙依赖动作电位(Ca-AP)时程缩短,并使Ca-AP的最大上升速率(Vmax)和幅值减小;安定还抑制兔与豚鼠心室乳头肌的收缩,相比之下对豚鼠的作用更明显。在戊脉安(2×10-6mol/L)作用下,兔心乳头肌Ga-AP逐渐消失。提高溶液中Ca2+的浓度可拮抗安定和戊脉安的作用。PK11195(1×10-6mol/L)可使安定对兔心乳头肌APD作用的剂量-反应曲线平行右移,且拮抗安定对Ca-AP的作用。预先加入PK11195(3×10-6mol/L),则戊脉安不能取消Ca-AP。上述结果提示。(1)兔心乳头肌存在的苯二氮(艹卓)结合位点具有外周型苯二氮(艹卓)受体(BZR)的性质;(2)这种受体的激活可导致钙内流减少;(3)BZR的密度及反应性可能存在种属差异。
【Abstract】 Effects of diazepam, verapamil and PK11195 on the action potential and con-tractility of the rabbit papillary muscle were investigated. Some comparisons werealso made between the effects of diazepam on the contractility of the rabbit andthe guinea pig. 0.7--22.4×10-6 mol/L diazapem shortened the duration of the action potential(APD) and calcium-dependent action potential(Ca-AP), and decreased the maxi-mum rise rate as well as the amplitude of the Ca-AP in the rabbit papillary muscle,which was accompanied by a decrease of contractility. The effect of diaz-epam on the contractility was more pronounced in the guinea pig. 2×10-6 mol/Lverapamil suppressed the Ca-AP of the rabbit papillary muscle, an effect thatcould be antagonized by increasing the external calcium concentration. Thecurve relating APD or contractility to diazepam dosage could be shifted to theright by 1×10-6 mol/L PK11195. In the presence of PK11195, the Ca-AP wasmore resistant to the effect of verapamil. Our experimental results suggest: (a) Benzodiazepine binding sites in therabbit papillary muscle may act as peripheral benzodiazepine receptors; (b) Activa-tion of these receptors can result in a decrease of calcium influx; (c) Speciesdifferences may exist in the density and responsibility of this receptor.
【Key words】 rabbit papillary muscle; benzodiazepine receptor; diazepam; PK 11195;
- 【文献出处】 生理学报 ,Acta Physiological Sinica , 编辑部邮箱 ,1987年04期
- 【被引频次】2
- 【下载频次】18